Seclidemstat (SP-2577)

Synonyms: SP-2577 mesylate

Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. Seclidemstat (SP-2577) has potential antineoplastic activity.

Seclidemstat (SP-2577) Chemical Structure

Seclidemstat (SP-2577) Chemical Structure

CAS No. 1423715-37-0

Purity & Quality Control

Seclidemstat (SP-2577) Related Products

Biological Activity

Description Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. Seclidemstat (SP-2577) has potential antineoplastic activity.
Targets
LSD1/KDM1A [1]
(Cell-free assay)
13 nM
In vitro
In vitro

The combination therapy of Seclidemstat (SP-2577) with checkpoint inhibitors may induce or augment immunogenic responses of SWI/SNF-mutated ovarian cancers. Seclidemstat promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in small cell carcinoma of the ovary hypercalcemic type (SCCOHT) cell lines. Seclidemstat (3 μM) promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line.[1]

Cell Research Cell lines Small cell carcinoma of the ovary hypercalcemic type (SCCOHT) cell lines, ovarian clear cell carcinomas (OCCC) cell lines
Concentrations 1μM,3 μM
Incubation Time 72 h
Method

The SCCOHT and OCCC cell lines are seeded in T-25 tissue culture treated flasks at 3 x 105 cells in 5mL of the appropriate phenol red free complete growth medium. After 48 h, at 70–80% confluency, the cells are treated with 3μM or 1μM of Seclidemstat. After 72 h, the media is collected from the flasks and stored at -80°C until use for various assays.

In Vivo
In vivo

SP-2577 (Seclidemstat) is an inhibitor of lysine-specific demthylase KDM1A (LSD1) potential antineoplastic activity against pediatric sarcomas.

Animal Research Animal Models C.B.17SC scid−/− female mice
Dosages 100 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04611139 Withdrawn
SCCOHT|Ovarian Clear Cell Tumor|Ovarian Endometrioid Adenocarcinoma|Endometrial Cancer
HonorHealth Research Institute|Merck Sharp & Dohme LLC|Salarius Pharmaceuticals LLC
December 31 2021 Phase 1
NCT03895684 Completed
Advanced Solid Tumors
Salarius Pharmaceuticals LLC
June 25 2019 Phase 1
NCT03600649 Active not recruiting
Ewing Sarcoma|Myxoid Liposarcoma|SarcomaSoft Tissue|Desmoplastic Small Round Cell Tumor|Extraskeletal Myxoid Chondrosarcoma|Angiomatoid Fibrous Histiocytoma|Clear Cell Sarcoma|Primary Pulmonary Myxoid Sarcoma|Myoepithelial Tumor|Sclerosing Epithelioid Fibrosarcoma|Fibromyxoid Tumor
Salarius Pharmaceuticals LLC|National Pediatric Cancer Foundation
June 4 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 450.94 Formula

C20H23ClN4O4S

CAS No. 1423715-37-0 SDF --
Smiles CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCN(CC2)C)C3=C(C=CC(=C3)Cl)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 90 mg/mL ( (199.58 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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